Pharmacological profile of a novel H₂S-releasing aspirin

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• 作者：Anna Sparatore ; Elena Perrino ; Valerio Tazzari ; Daniela Giustarini ; Ranieri Rossi ; Giuseppe Rossoni ; Kati Erdman ; Henning Schrö ; der ; Piero Del Soldato
• 关键词：Aspirin ; Hydrogen sulfide ; Dithiolethione ; Thromboxane ; Glutathione ; Heme oxygenase-1 ; Free radicals
• 刊名：Free Radical Biology and Medicine
• 出版年：2009
• 出版时间：1 March 2009
• 年：2009
• 卷：46
• 期：5
• 页码：586-592
• 全文大小：566 K

文摘

The pharmacological profile of a new, safe, and effective hydrogen sulfide (H₂S)-releasing derivative of aspirin (ACS14) is described. We report the synthesis of ACS14, and of its deacetylated metabolite (ACS21), the preliminary pharmacokinetics, and its in vivo metabolism, with the H₂S plasma levels after intravenous administration in the rat. ACS14 maintains the thromboxane-suppressing activity of the parent compound, but seems to spare the gastric mucosa, by affecting redox imbalance through increased H₂S/glutathione formation, heme oxygenase-1 promoter activity, and isoprostane suppression.